| Drug ID: | Drug112 |
|---|---|
| Drug Name: | Tofacitinib |
| CID: | 9926791 |
| DrugBank ID: | DB08895 |
| Modality: | Small Molecule |
| Groups: | approved |
| US Approved: | YES |
| Other Approved: | YES |
| Identifier: | NCT00787202, , NCT03281304, , NCT01458574, , NCT01470612, , NCT06625450, , NCT04424303, , NCT05112263, , NCT06095128, , NCT05728008, , NCT05431283, , NCT05313620, , NCT04925973, , NCT06780683, , NCT06274996, , NCT05782907, , NCT06095596, , NCT03653026, , NCT02819635, , NCT03345836, , NCT03006 |
| Molecular Formula: | C16H20N6O |
| Molecular Weight: | 312.37 g/mol |
| Isomeric SMILES: | C[C@@H]1CCN(C[C@@H]1N(C)C2=NC=NC3=C2C=CN3)C(=O)CC#N |
| Synonyms: | Tofacitinib; 477600-75-2; 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile; Cp-690 free base; tofacitinibum; UNII-87LA6FU830; CHEBI:71200; 87LA6FU830; CP-690550 FREE BASE; CP-690,550 FREE BASE |
| Phase 0: | 6 |
| Phase 1: | 84 |
| Phase 2: | 131 |
| Phase 3: | 80 |
| Phase 4: | 39 |
| Description: | Tofacitinib is an inhibitor of Janus kinases, a group of intracellular enzymes involved in signaling pathways that affect hematopoiesis and immune cell function. It is approved by the FDA for treatment of moderate to severe rheumatoid arthritis that responds inadequately to methotrexate or in those who are intolerant to methotrexate. Besides rheumatoid arthritis, tofacitinib has also been studied in clinical trials for the prevention of organ transplant rejection, and the treatment of psoriasis and ulcerative colitis. Known adverse effects include nausea and headache as well as more serious immunologic and hematological adverse effects. Tofacitinib is marketed under the brand name Xeljanz. |
Molecular Structure
Knowledge Graph
| dtID | CID | Compound Name | Gene ID | Gene Name | Species | PubMed IDs | Action |
|---|---|---|---|---|---|---|---|
| dt948 | 9926791 | Tofacitinib | 2048 | EPHB2 | Homo sapiens (human) | Inhibitor | |
| dt949 | 9926791 | Tofacitinib | 6777 | STAT5B | Homo sapiens (human) | None | |
| dt950 | 9926791 | Tofacitinib | 3716 | JAK1 | Homo sapiens (human) | Inhibitor | |
| dt951 | 9926791 | Tofacitinib | 3718 | JAK3 | Homo sapiens (human) | None | |
| dt952 | 9926791 | Tofacitinib | 29110 | TBK1 | Homo sapiens (human) | 25540906 | None |
| dt953 | 9926791 | Tofacitinib | 3717 | JAK2 | Homo sapiens (human) | 24417533 | Inhibition |
| dt954 | 9926791 | Tofacitinib | 3718 | JAK3 | Homo sapiens (human) | Inhibition | |
| dt955 | 9926791 | Tofacitinib | 3718 | JAK3 | Homo sapiens (human) | 24417533 | Inhibition |
| dt956 | 9926791 | Tofacitinib | 3718 | JAK3 | Homo sapiens (human) | 27572962 | Inhibition |
| dt957 | 9926791 | Tofacitinib | 3716 | JAK1 | Homo sapiens (human) | 24417533 | Inhibition |
- No data available
Phase Distribution
Phase Description
- Phase 0: Exploratory trials to assess drug behavior in humans
- Phase 1: Safety trials to determine safe dosage range
- Phase 2: Efficacy trials to evaluate therapeutic effects
- Phase 3: Large-scale trials to confirm efficacy and safety
- Phase 4: Post-marketing surveillance for long-term safety and efficacy
| Trial ID | Title | Phase | Status | Sponsor | Indications | Interventions | |
|---|---|---|---|---|---|---|---|
| NCT05431283 | Real-world Effectiveness of Tofacitinib on Ulcerative Colitis Associated Spondyloarthropathy | NULL | UNKNOWN | Italian Group for the study of Inflammatory Bowel Disease (IG-IBD) | Ulcerative Colitis|Spondyloarthropathy | DRUG: Tofacitinib | Details |
| NCT05313620 | Effect of Tofacitinib on Coagulation and Platelet Function, and Its Role in Thromboembolic Events | PHASE4 | RECRUITING | Fundación de Investigación Biomédica - Hospital Universitario de La Princesa | Ulcerative Colitis|Thromboembolism | DRUG: Tofacitinib|DRUG: Infliximab Adalimumab y G… | Details |
| NCT07138898 | Immunosuppressant Management in Rheumatology Patients Undergoing Elective Total Shoulder Arthroplasty | PHASE2 | NOT_YET_RECRUITING | NYU Langone Health | Rheumatic Disease | DRUG: Methotrexate|DRUG: Sulfasalazine|DRUG: Hydr… | Details |
| NCT05186623 | Prediction Model for Response to Biologics and Small Molecular Agent for UC | NULL | RECRUITING | Asan Medical Center | Ulcerative Colitis | DRUG: Vedolizumab, Ustekinumab, or Tofacitinib | Details |
| NCT05112263 | Tofacitinib Versus Cyclosporine for Steroid Refractory Acute Severe Ulcerative Colitis | NA | NOT_YET_RECRUITING | Post Graduate Institute of Medical Education and Research, Chandigarh | Ulcerative Colitis | DRUG: Tofacitinib|DRUG: Cyclosporine | Details |
| NCT05104723 | Safety and Efficacy of Tofacitinib for Chronic Granulomatous Disease With Inflammatory Complications | PHASE1|PHASE2 | ENROLLING_BY_INVITATION | National Institute of Allergy and Infectious Diseases (NIAID) | Chronic Granulomatous Disease|Inflammatory Gastro… | DRUG: XELJANZ (tofacitinib) | Details |
| NCT05082428 | This Study is to Describe and Evaluate Patients in Finland Treated With Tofacitinib for the Treatment of Ulcerative Colitis Using Real World Data. | NULL | COMPLETED | Pfizer | Ulcerative Colitis | None | Details |
| NCT05069259 | Generate Real World Data On Tofacitinib Induction Therapy and Changes In Clinical and Patient Reported Outcomes. | NULL | TERMINATED | Pfizer | Ulcerative Colitis | OTHER: Stool sample collection | Details |
| NCT04925973 | Tofacitinib for Hospitalized Acute Severe Ulcerative Colitis Management | PHASE2 | ACTIVE_NOT_RECRUITING | McMaster University | Ulcerative Colitis Acute | DRUG: Tofacitinib 10 MG [Xeljanz] | Details |
| NCT04743518 | Impact of Anti-TNF, Vedolizumab and Tofacitinib on Aortic Stiffness, Carotid Intima-media Thickness and Cardiovascular Risk of Patients With Ulcerative Colitis | PHASE4 | RECRUITING | Centre Hospitalier Universitaire, Amiens | Ulcerative Colitis | OTHER: Aortic pulse wave velocity|OTHER: carotid … | Details |
| NCT04624230 | Evaluation of Oral Tofacitinib in Children Aged 2 to 17 Years Old Suffering From Moderate to Severe Ulcerative Colitis | PHASE3 | ACTIVE_NOT_RECRUITING | Pfizer | Ulcerative Colitis | DRUG: tofacitinib | Details |
| NCT04424303 | Tofacitinib in Adult Patients With Moderate to Severe Ulcerative Colitis | NULL | COMPLETED | Pfizer | Ulcerative Colitis | DRUG: Tofacitinib | Details |
| NCT04338204 | Observational Study To Assess The Effectiveness and Treatment Adherence Of Tofacitinib of Ulcerative Colitis In Clinical Practice In Sweden | NULL | RECRUITING | Pfizer | Ulcerative Colitis | DRUG: tofacitinib | Details |
| NCT04032756 | Tofacitinib Registry of Patients With Ulcerative Colitis in Germany | NULL | TERMINATED | Ced Service GmbH | Colitis, Ulcerative|Biologics|Tofacitiniib|Chroni… | None | Details |
| NCT03885713 | Identification of Predictive Biomarkers for Response to Biologic Therapies and Tofacitinib in Inflammatory Bowel Disease | PHASE4 | COMPLETED | Fundación de Investigación Biomédica - Hospital Universitario de La Princesa | Inflammatory Bowel Diseases|Crohn Disease|Ulcerat… | BIOLOGICAL: Infliximab or adalimumab or golimumab… | Details |
| NCT03772145 | Tofacitinib Response in Ulcerative Colitis - a Real World Prospective Multi-center Study | NULL | TERMINATED | University of North Carolina, Chapel Hill | Ulcerative Colitis | None | Details |
| NCT03663400 | Identify Predictors That Distinguish Between Tofacitinib Responders and Non-responders Based on Genotype and Cellular and Molecular Profiles From Pinch Biopsies, Blood and Stool Samples | NULL | COMPLETED | NYU Langone Health | Ulcerative Colitis | DIAGNOSTIC_TEST: GWAS analysis by Illumina BeadCh… | Details |
| NCT03591770 | Shingrix Vaccine in Patients With Moderate to Severe Ulcerative Colitis on Tofacitinib | PHASE4 | TERMINATED | Boston Medical Center | Inflammatory Bowel Diseases | BIOLOGICAL: SHINGRIX | Details |
| NCT03281304 | A Study of Tofacitinib in Patients With Ulcerative Colitis in Stable Remission | PHASE4 | TERMINATED | Pfizer | Ulcerative Colitis | DRUG: CP-690,500 5 mg|DRUG: CP-690,550 10 mg | Details |
| NCT03103412 | TD-3504 SAD in Healthy Subjects and Subjects With Ulcerative Colitis (UC) | PHASE1 | COMPLETED | Theravance Biopharma | Active Mild Ulcerative Colitis, Active Moderate U… | DRUG: TD-3504|DRUG: 15N2-tofacitinib|DRUG: Placebo | Details |
| Disease ID | Disease Name | Definition | Category | Related Drugs | Mechanism | |
|---|---|---|---|---|---|---|
| No data available | ||||||
| Strategy ID | Therapeutic Strategy | Synonyms | Related Drugs | Mechanism | |
|---|---|---|---|---|---|
| S07 | Blockade of cytokine | Cytokine signalling | apremilast; roflumilast; filgotinib; tofacitinib; ABT494; ABT-874; ustekinumab; isankizumab; LY-2525623; AMG139; MEDI2079; guselkumab | Various T-cell subsets, their differentiation pathways and … | Details |
Real-world evidence of tofacitinib effectiveness and safety in patients with re…
PMID: 31732444
Year: 2020
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Phase III trials demonstrated effectiveness of tofacitinib, an oral Janus kinase inhibitor, to induce and maintain remission in patients …
Multiple esophageal ulcers due to tofacitinib 10 mg twice daily for ulcerative …
PMID: 31705375
Year: 2020
Relationship Type:
Treatment
Score: 6.5
A 26-year-old man was admitted to our institution for ulcerative colitis treatment. He used mesalamine, steroid, immunomodulators, and anti-TNFalpha …
Efficacy and safety of tofacitinib dose de-escalation and dose escalation for p…
PMID: 31660640
Year: 2020
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: For patients with UC, flexible maintenance dosing therapy may confer advantages for safety, efficacy, costs and patient preference. Tofac…
Off-label studies on tofacitinib in dermatology: a review
PMID: 31581859
Year: 2021
Relationship Type:
Treatment
Score: 6.5
PURPOSE: Tofacitinib citrate is an oral Janus kinase 1/3 inhibitor approved for rheumatoid arthritis, ulcerative colitis, and active psoriatic arthri…
Evaluating tofacitinib citrate in the treatment of moderate-to-severe active ul…
PMID: 31118734
Year: 2019
Relationship Type:
Treatment
Score: 6.5
The etiology of ulcerative colitis (UC) is complex and involves a host of genetic, epigenetic and environmental factors. Over the last thirty years, …
The use of Tofacitinib in the treatment of inflammatory bowel disease
PMID: 31094180
Year: 2019
Relationship Type:
Treatment
Score: 6.5
Major advances in pharmacology of the 21st century include the development of a new class of drugs, which are low-molecular, chemically synthesized m…
A JAK1 Selective Kinase Inhibitor and Tofacitinib Affect Macrophage Activation …
PMID: 30668755
Year: 2019
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Janus kinases (JAKs) mediate cytokine signaling involved in inflammatory bowel disease. The pan-JAK inhibitor tofacitinib has shown effic…
Long-term safety and tolerability of oral tofacitinib in patients with Crohn's …
PMID: 30663107
Year: 2019
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Tofacitinib is an oral, small molecule Janus kinase inhibitor that is being investigated for inflammatory bowel disease. AIMS: This 48-we…
Safety of Tofacitinib for Treatment of Ulcerative Colitis, Based on 4.4 Years o…
PMID: 30476584
Year: 2019
Relationship Type:
Treatment
Score: 6.5
BACKGROUND & AIMS: Tofacitinib is an oral, small-molecule inhibitor of JAK approved in several countries for the treatment of ulcerative colitis (UC)…
Efficacy of Induction Therapy With High-Intensity Tofacitinib in 4 Patients Wit…
PMID: 30458248
Year: 2019
Relationship Type:
Treatment
Score: 6.5
As many as 25% of patients diagnosed with ulcerative colitis are hospitalized with an episode of acute severe ulcerative colitis (ASUC).(1) The stand…
Tofacitinib for the treatment of ulcerative colitis
PMID: 30285500
Year: 2018
Relationship Type:
Treatment
Score: 6.3
New generations of small molecules are being developed for the treatment of ulcerative colitis. Among them, tofatinib (a Janus kinase (JAK) inhibitor…
TOFACITINIB IN THE MANAGEMENT OF ULCERATIVE COLITIS REFRACTORY TO ANTI-TNF AND …
PMID: 30043874
Year: 2018
Relationship Type:
Treatment
Score: 6.3
Janus kinases inhibitors have already been incorporated into the management of immune-mediated diseases, such as rheumatoid arthritis, and are being …
Outcomes of Pregnancies With Maternal/Paternal Exposure in the Tofacitinib Safe…
PMID: 29982686
Year: 2018
Relationship Type:
Treatment
Score: 6.3
BACKGROUND: Active inflammatory bowel disease increases the risk of adverse pregnancy outcomes. Tofacitinib is an oral, small molecule Janus kinase i…
Herpes Zoster Infection in Patients With Ulcerative Colitis Receiving Tofacitin…
PMID: 29850873
Year: 2018
Relationship Type:
Treatment
Score: 6.3
BACKGROUND: Tofacitinib is an oral, small molecule Janus kinase inhibitor that is being investigated for ulcerative colitis (UC). Tofacitinib is appr…
The use of tofacitinib in the treatment of inflammatory bowel disease
PMID: 29701124
Year: 2018
Relationship Type:
Treatment
Score: 6.3
Janus kinases (JAK) play a major role in the immunologic pathways and specifically in signal transduction in inflammatory bowel disease. Thus, they c…
Exposure-response characterization of tofacitinib efficacy in moderate to sever…
PMID: 29377257
Year: 2018
Relationship Type:
Treatment
Score: 6.3
AIMS: Tofacitinib is an oral, small molecule JAK inhibitor being investigated for ulcerative colitis (UC). In a phase 2 dose-ranging study, tofacitin…
Tofacitinib in Patients with Ulcerative Colitis: Health-Related Quality of Life…
PMID: 29028981
Year: 2018
Relationship Type:
Treatment
Score: 6.3
BACKGROUND AND AIMS: Tofacitinib is an oral, small molecule Janus kinase [JAK] inhibitor that is being investigated for ulcerative colitis [UC]. We e…
Tofacitinib as Induction and Maintenance Therapy for Ulcerative Colitis
PMID: 28467869
Year: 2017
Relationship Type:
Treatment
Score: 6.3
BACKGROUND: Tofacitinib, an oral, small-molecule Janus kinase inhibitor, was shown to have potential efficacy as induction therapy for ulcerative col…
Tofacitinib for the treatment of tumor necrosis factor-α inhibitor refractory e…
PMID: 27663846
Year: 2016
Relationship Type:
Treatment
Score: 6.3
BACKGROUND: Esophageal Crohn's disease is reported as a rare manifestation, although its prevalence may be underestimated because upper endoscopies a…
Direct and Indirect Effects of Tofacitinib on Treatment Satisfaction in Patient…
PMID: 27194530
Year: 2016
Relationship Type:
Treatment
Score: 6.3
BACKGROUND AND AIMS: This mediation modelling analysis evaluated direct and indirect effects of tofacitinib, an oral, small molecule Janus kinase inh…